AZD-3463 ALK/IGF1R inhibitor|cas:1356962-20-3|西域试剂

AZD-3463 ALK/IGF1R inhibitor,99.96%

产品编号：Bellancom-15609| CAS NO：1356962-20-3| 分子式：C₂₄H₂₅ClN₆O| 分子量：448.95

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货号	价格	库存与货期
Bellancom-15609	￥550.00	杭州北京（现货）
Bellancom-15609	￥850.00	杭州北京（现货）
Bellancom-15609	￥3600.00	杭州北京（现货）
Bellancom-15609	￥5400.00	杭州北京（现货）

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AZD-3463 ALK/IGF1R inhibitor

产品介绍

AZD-3463 (ALK/IGF1R inhibitor) 是一种具有口服活性的 ALK/IGF1R 抑制剂，对 ALK 作用的 K_i 值为 0.75 nM。AZD-3463 可诱导神经母细胞瘤细胞凋亡 (apoptosis) 和自噬 (autophagy)。

生物活性

AZD-3463 (ALK/IGF1R inhibitor) is an orally active ALK/IGF1R inhibitor, with a K_i of 0.75 nM for ALK. AZD3463 induces apoptosis and autophagy in neuroblastoma cells.

体外研究

AZD-3463 (0-50 µM; 72 h) suppresses the viability and proliferation of both wild type and mutant ALK NB cells.
AZD-3463 (10 µM; 0-4 h) effectively inhibits ALK-mediated PI3K/AKT/mTOR signaling and induces apoptosis and autophagy in NB cells.
AZD-3463 (0-100 nM; 4 h) inhibits FLT3-ITD-mediated activation of AKT, ERK1/2 and p38 in a dose-dependent manner in MOLM-13 and MV4-11 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	IMR-32, NGP, NB-19, SH-SY5Y, SK-N-AS and LA-N-6 cells
Concentration:	0-50 µM
Incubation Time:	72 h
Result:	Inhibited IMR-32, NGP, NB-19, SH-SY5Y, SK-N-AS and LA-N-6 cells with IC₅₀ values of 2.802, 14.55, 11.94, 1.745, 21.34 and 16.49 µM, respectively.

Cell Autophagy Assay

Cell Line:	IMR-32, NGP , SH-SY5Y and SK-N-AS cells
Concentration:	10 µM
Incubation Time:	0-4 h
Result:	Potently inhibited or totally abolished the phosphorylation of Akt Ser473 and RPS6 Thr235/236. Induced cleavage of the autophagy marker LC3 A/BΙΙ within four hours.

Apoptosis Analysis

Cell Line:	MOLM-13 and MV4-11 cells
Concentration:	0-100 nM
Incubation Time:	4 h (pretreat)
Result:	Selectively inhibited FLT3-ITD but not ligand-induced wild-type FLT3.

体内研究
(In Vivo)

AZD3463 (15 mg/kg; i.p.; once daily for 2 days) inhibits tumor growth in different orthotopic NB xenograft mouse models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5 to 6-week-old female athymic Ncr nude mice (SH-SY5Y and NGP xenograft tumors bearing mice).
Dosage:	15 mg/kg
Administration:	Intraperitoneal injection; once daily for 2 days
Result:	Showed anti-tumor efficacy in both ALK WT and F1174L mutant orthotropic xenograft mouse models of NB.

体内研究

AZD3463 (15 mg/kg; i.p.; once daily for 2 days) inhibits tumor growth in different orthotopic NB xenograft mouse models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5 to 6-week-old female athymic Ncr nude mice (SH-SY5Y and NGP xenograft tumors bearing mice).
Dosage:	15 mg/kg
Administration:	Intraperitoneal injection; once daily for 2 days
Result:	Showed anti-tumor efficacy in both ALK WT and F1174L mutant orthotropic xenograft mouse models of NB.

体内研究

AZD3463 (15 mg/kg; i.p.; once daily for 2 days) inhibits tumor growth in different orthotopic NB xenograft mouse models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	5 to 6-week-old female athymic Ncr nude mice (SH-SY5Y and NGP xenograft tumors bearing mice).
Dosage:	15 mg/kg
Administration:	Intraperitoneal injection; once daily for 2 days
Result:	Showed anti-tumor efficacy in both ALK WT and F1174L mutant orthotropic xenograft mouse models of NB.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (44.55 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2274 mL	11.1371 mL	22.2742 mL
5 mM	0.4455 mL	2.2274 mL	4.4548 mL
10 mM	0.2227 mL	1.1137 mL	2.2274 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (4.45 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.45 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液